The invention relates to a pharmaceutical preparation for oral administration which contains Tolperison or a salt thereof.
Tolperison-containing drugs are known in various preparation forms. Thus EP 0 295 411 B describes a pharmaceutical preparation for percutaneous administration of Tolperison or a salt thereof.
Other forms of administration of Tolperison-containing drugs are also known. Thus JP 51091315 A describes a stable syrup of Tolperison which is intended for oral administrations.
Tolperison is the international generic name for the muscle relaxant (RS)-2,4xe2x80x2-dimethyl-3-piperidonopropriophenone) with the empirical formula C16H23NO.
Tolperison and its salts are known as an agent for improving not only different symptoms with respect to spastic paralysis, but also muscle tone which originates from diseases such as cervical syndrome, inflammation of the joints and back pain.
The disadvantage in oral administration of Tolperison or a salt thereof is that the action quickly diminishes so that Tolperison-containing preparations must be taken several times daily and that the gastrointestinal tract of the patient can be damaged.
The disadvantage of percutaneous use, as is known from EP 0 295 411 B, is the only inadequate percutaneous absorption of the pharmaceutical active ingredient, Tolperison.
The active ingredient Tolperison is present as a 50/50 racemate. Studies have shown that up to 90% of the (xe2x88x92) isomer and up to only 10% of the (+) isomer of Tolperison are present in the blood. For a long time it had not been conclusively clarified whether the 90/10 racemate present in the blood (of humans) is formed by re-racemization or by intensified resorption of the (xe2x88x92) isomer.
The object of the invention is to make available a preparation which contains Tolperison or a salt thereof which can be orally administered without the disadvantages of the known orally administered preparations of Tolperison occurring.
This object is achieved as claimed in the invention with a preparation which is characterized in claim 1.
Preferred and advantageous embodiments of the preparation as claimed in the invention are the subject matter of the dependent claims.
The preparation as claimed in the invention replaces the action which rapidly fades in the known oral preparations of Tolperison or its salts by a long lasting action since the preparation is produced such that the active ingredient Tolperison or the salt thereof is released only on a delayed basis. In particular, in the preparation as claimed in the invention it can be advantageous that the delay of the release of the active ingredient Tolperison is set such that the Tolperison is resorbed predominantly in the intestine.
The advantages of controlled release of pharmaceutical active ingredients are well known in the area of pharmaceuticals and consist among others in that the desired content of the active ingredient in the blood can be maintained over a comparatively long time interval so that the patient is no longer compelled to take a drug several times daily.
The preparations as claimed in the invention with delayed release of Tolperison or salts thereof can be present for example in combination with various hydrogels which can be of synthetic, semisynthetic or natural origin.
Oral preparations with delayed release of the active ingredientxe2x80x94here Tolperison or a salt thereofxe2x80x94should be adjustable such that the release rates and profiles can be set according to the physiological and chronotherapeutic requirements. This is allowed by the preparation as claimed in the invention. Studies have shown that the (xe2x88x92) isomer and the (+) isomer of Tolperison are almost identically effective. Therefore racemic mixtures of the isomers of Tolperison are also essentially identically active as one or the other isomer alone.
Tolperison can be present in the preparations as claimed in the invention as a 50/50 racemate or as a racemic mixture which differs from the 50/50 racemate. Racemates in which the content of the (xe2x88x92) isomer is higher than that of the (+) isomer are likewise used. Racemates with a predominant proportion of the (xe2x88x92) isomer of Tolperison (2,4xe2x80x2-dimethyl-3-piperidonopropriophenone) can be present as 90/10 racemates.
Examples of pharmaceutical preparations as claimed in this invention are given below.